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| Targets |
1-(2-Pyridyl)piperazine functions as a selective antagonist of α2-adrenergic receptors. By blocking α2-adrenoceptors, it exhibits sympatholytic activity, which may lead to vasodilation and decreased sympathetic nervous system output. The compound has been identified as a metabolite of azaperone, a butyrophenone neuroleptic used in veterinary medicine. Its receptor binding profile makes it useful in pharmacological research studying adrenergic signaling pathways.
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| ln Vitro |
1-(2-Pyridyl)piperazine functions as a selective antagonist of α2-adrenergic receptors. It displays empathetic behavior. It is an Azaperone metabolite as well.
In vitro studies have characterized 1-(2-pyridyl)piperazine as a selective α2-adrenoceptor antagonist. The compound shows sympatholytic activity in various in vitro assay systems. It is employed as a reagent for the determination of aliphatic and aromatic isocyanates in air by reversed-phase HPLC and for the fluorometric determination of airborne diisocyanates. These applications demonstrate its utility in both pharmacological and analytical chemistry research. |
| ln Vivo |
No specific in vivo pharmacological activity data for 1-(2-pyridyl)piperazine as a standalone drug have been extensively documented. As a metabolite of azaperone, its in vivo effects would be related to the pharmacological profile of the parent drug. In animal studies, the compound would be expected to exhibit α2-adrenoceptor antagonism with sympatholytic effects. Dosing and administration would follow standard protocols for adrenergic receptor antagonist studies.
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| Enzyme Assay |
For non-cellular receptor binding assays, 1-(2-pyridyl)piperazine can be evaluated for its affinity at α2-adrenoceptors using radioligand binding techniques. Typical protocols involve incubating the compound with membrane preparations expressing α2-adrenergic receptors and a radiolabeled ligand such as [3H]-rauwolscine or [3H]-RX821002. Non-specific binding is determined in the presence of an excess of unlabeled competitor. Binding affinity (Ki) is calculated from competition curves. Assays are performed in appropriate buffer systems at 25°C or 37°C.
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| Cell Assay |
For in vitro cell-based studies, 1-(2-pyridyl)piperazine can be dissolved in DMSO or aqueous buffers and diluted in cell culture medium. Cells expressing α2-adrenergic receptors (such as neuronal cell lines or transfected HEK-293 cells) are treated with the compound to assess receptor antagonism. Functional assays may measure downstream signaling events such as cAMP accumulation or calcium mobilization. The compound is typically tested at concentrations ranging from nanomolar to micromolar depending on the assay system.
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| Animal Protocol |
For in vivo animal studies, 1-(2-pyridyl)piperazine can be administered via various routes including intraperitoneal, intravenous, or oral administration. Dosing solutions should be prepared fresh using appropriate vehicles such as saline or DMSO-based formulations. The compound should be handled with care as it is an irritant. Dosing regimens and administration protocols should follow approved animal welfare guidelines and institutional protocols for adrenergic receptor studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 1-(2-pyridyl)piperazine: the compound has a molecular weight of 163.22, pKa of 8.63±0.10, and water solubility >500 g/L at 20°C. It is soluble in chloroform and methanol. The compound is sensitive to air and should be stored in a flammable area. Appearance: clear colorless to yellow liquid. Storage: flammables area, protected from air and moisture. Detection methods: GC and NMR.
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| Toxicity/Toxicokinetics |
Toxicological data for 1-(2-pyridyl)piperazine indicate it is an irritant. Hazard codes: Xi (irritant). Risk statements: R36/37/38 (irritating to eyes, respiratory system, and skin). Safety statements: S26 (in case of contact with eyes, rinse immediately with plenty of water and seek medical advice), S36 (wear suitable protective clothing). RIDADR: 2735, WGK Germany: 3, Hazard Class: 8. The compound is for research use only.
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| Additional Infomation |
1-(2-Pyridyl)piperazine is a compound in which trans-cinnamic acid is substituted at the 3-position of the benzene ring with a dihydroxy(oxo)-5-antimonyyl group. It is an anti-HIV-1 drug. It belongs to the cinnamic acid class of compounds and is also an antimony oxoacid. It is a metabolite of buspirone and gaperazone.
1-(2-Pyridyl)piperazine (CAS 34803-66-2) is a selective α2-adrenoceptor antagonist with sympatholytic activity. It is a metabolite of azaperone (A802200). The compound is used as a reagent for the determination of isocyanates in air by HPLC and fluorometric methods. It has a BR number of 140423 and an HS code of 29339900. No clinical trials or human therapeutic approvals exist; the product is for research use only. |
| Molecular Formula |
C9H13N3
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| Molecular Weight |
163.22
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| Exact Mass |
163.11
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| CAS # |
34803-66-2
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| PubChem CID |
94459
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| Appearance |
Colorless to light yellow liquid（Density：1.072 g/cm3）
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
314.4±22.0 °C at 760 mmHg
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| Melting Point |
92-94
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| Flash Point |
143.9±22.3 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.547
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| LogP |
0.19
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
12
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| Complexity |
132
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=NC(=C1)N2CCNCC2
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| InChi Key |
GZRKXKUVVPSREJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H13N3/c1-2-4-11-9(3-1)12-7-5-10-6-8-12/h1-4,10H,5-8H2
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| Chemical Name |
1-pyridin-2-ylpiperazine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.1267 mL | 30.6335 mL | 61.2670 mL | |
| 5 mM | 1.2253 mL | 6.1267 mL | 12.2534 mL | |
| 10 mM | 0.6127 mL | 3.0634 mL | 6.1267 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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